Increasing Dissolution Rates and Gastrointestinal Absorption of Drugs Via Solid Solutions and Eutectic Mixtures IV

The purpose of the study was to improve the physicochemical properties of Mesalamine like solubility and dissolution rate by forming solid dispersions with sodium lauryl sulphate (SLS) and Urea (UR) as water-soluble carriers. The solid dispersion of Mesalamine by kneading method were prepared using 1:1, 1:2 and 1:3 ratios of drug to polymer using methanol as solvent. Characterization of Mesalamine solid dispersion was performed by Fourier Transform Infrared (FTIR) spectroscopy and X-ray powder diffractometry study. FTIR spectra reveal that there was no drug -carrier interaction and absence of Mesalamine peaks in XRD profile suggests the transformation of crystalline Mesalamine to amorphous form. The saturation Solubility study was carried out by using flask shaker method at room temperature. Dissolution study was conducted in 0.1N HCl at 37 o C ± 0.5 o C using USP type II (paddle) type dissolution apparatus. The prepared dispersion showed marked increase the saturation solubility and dissolution rate of Mesalamine than that of drug alone. Therefore the dissolution rate of poorly water soluble drug Mesalamine can be significantly enhanced by the preparation of solid dispersion using SLS and UR by kneading technique. INTRODUCTION:Mesalamine is 5-amino salicylic acid, active moiety of sulphasalazine. Its major indications are to treat mild to moderate acute exacerbations of ulcerative colitis's in remission, particularly in patients intolerant of sulphasalazine. It is white to pinkish crystals slightly soluble in water, 20 to 30 % absorbed following oral administrations.

Section: Introductionmentioning

confidence: 91%

Untitled

2011

“…It was estimated that 40% of active new chemical entities (NCEs) identified in combinatorial screening programs employed by many pharmaceutical companies are poorly water soluble and not well absorbed after oral administration 2,3 which can distract from the drugs inherent efficacy [4][5][6] .…”

Section: Introductionmentioning

confidence: 99%

Untitled

2012

Solubility is an important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Among all newly discovered chemical entities most of the drugs are lipophillic and fail to reach market due to their poor water solubility. The solubility behavior remains one of the most challenging aspect informational development. Hence various techniques are used for the improvement of solubility of poorly water soluble drugs which include micronization, chemical modification, pH adjustment, solid dispersion, complexation, co-solvency micellar solubilization, hydrotrophy etc. Of all these approaches solid dispersion have attracted tremendous interest as an efficient means of improving the dissolution rate and hence the bioavailability to arrange of hydrophobic drugs. This article reviews the various preparation techniques and types of solid dispersion based on molecular arrangement. Finally some of the practical aspects have also been considered for the preparation of dispersions.

“…Therefore, most of the new chemical entities under development these days are intended to be used as a solid dosage form that originate an effective reproducible in vivo plasma concentration after oral administration 3,4 . In fact, most new chemical entities are poorly soluble drugs, not wellabsorbed after oral administration 4,5 , which can distract from the drug's inherent efficacy [6][7][8] .…”

Section: Introductionmentioning

confidence: 99%

Untitled

2010

The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.